137473-27-9

Upstream product

• 64-17-5 ethanol 
• 5345-30-2 3-(4-methanesulfonyl-phenyl)-acrylic acid 
• 5398-77-6 para-methanesulfonylbenzaldehyde 
• 197905-49-0 4‐methoxy‐N‐(4‐(methylsulfonyl)benzylidene)aniline 
• 24045-02-1 (benzothiazole-2-sulfonyl)-acetic acid ethyl ester 
• 97410-25-8 1-(methylsulfonyl)-4-vinyl-benzene 
• 4114-31-2 ethylhydrazine carboxylate 
• 100515-19-3 1-(1,1-dimethoxy-methyl)-4-methanesulfonyl-benzene 
• 3446-89-7 4-(Methylthio)benzaldehyde 
• 100515-17-1 1-(1,1-dimethoxy-methyl)-4-methylsulfanyl-benzene 
• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 

Downstream Products

• 5345-30-2 3-(4-methanesulfonyl-phenyl)-acrylic acid 
• 1373543-38-4 ethyl (2R,3S)-2,3-dihydroxy-3-[4-(methylsulfonyl)phenyl]propanoate 
• 1373543-40-8 ethyl (2R,3S)-3-hydroxy-3-[4-(methylsulfonyl)phenyl]-2-{[(4-nitrophenyl)sulfonyl]oxy}propanoate 
• 41917-86-6 trans-4-(methylsulfonyl)cinnamaldehyde 
• 125872-64-2 (E)-3-[4-(methylsulfonyl)phenyl]prop-2-en-1-ol 

Relevant academic research and scientific papers

Oxidative alkoxycarbonylation of terminal alkenes with carbazates

A range of terminal alkenes smoothly underwent palladium-catalyzed oxidative alkoxycarbonylation with carbazates under an oxygen atmosphere to afford structurally diverse α,β-unsaturated esters in moderate to good yields with excellent regioselectivity and E selectivity.

An efficient enantioselective synthesis of florfenicol based on sharpless asymmetric dihydroxylation

An efficient and highly enantioselective synthesis of florfenicol- via a new intermediate threo-dihydroxy ester, with a Sharpless asymmetric dihydroxylation as the key step, is reported. A ring-opening/reduction strategy avoids the formation of a chlorinated byproduct that occurs in Schumachers phenyloxazoline procedure. The overall yield of florfenicol by this new process is 23% based on 4-(methylsulfonyl)benzaldehyde. Georg Thieme Verlag Stuttgart · New York.

Stereoselective olefination and regiospecific vicinal difunctionalization of imines with α-(benzothiazol-2-ylsulfonyl) carbonyl compounds

Depending on their structures, imines are able to undergo either olefination or vicinal difunctionalization with various α-(benzothiazol-2- ylsulfonyl) carbonyl compounds in the absence of external bases. The olefination reaction of aromatic imines with α-(benzothiazol-2-ylsulfonyl) carbonyl compounds proceeds smoothly in tetrahydrofuran at 70 °C to give structurally diverse α,β-unsaturated esters, amides, and ketones in good to excellent yields and with extremely high (E) selectivity. In contrast, the carbon-nitrogen double bonds of cyclic imines and the carbon-carbon double bonds of α,β-unsaturated imines are subjected to regiospecific vicinal difunctionalization with α-(benzothiazol-2-ylsulfonyl) carbonyl compounds under the same reaction conditions to give a variety of benzothiazole derivatives in good to excellent yields. It is noteworthy that the benzothiazole moiety is present in a number of antitumor agents and bioluminescent molecules. In addition, plausible reaction pathways have been proposed to account for these transformations, and these are substantially supported by ESI-MS analysis of the reaction mixtures.

Amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes

Novel amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

Synthesis and antifungal activities of R-102557 and related dioxane- triazole derivatives

Novel triazole compounds with a dioxane ring were synthesized. Condensation of the diol precursor 10 with various aromatic aldehydes 11 - 13 under acidic conditions afforded a series of dioxane-triazole compounds 14 - 16. The antifungal activities of the compounds 14 - 16 were evaluated in vivo in mice infection models against Candida and Aspergillus species. High activities were seen for the derivatives with one or two double bond(s) and an aromatic ring substituted with an electron-withdrawing group in the side chain. Among the derivatives, R-102557 (16R: Ar=4-(2,2,3,3- tetrafluoropropoxy)phenyl) showed excellent in vivo activities against Candida, Aspergillus and Cryptococcus species. It also showed high tolerance in a preliminary toxicity study in rats.

BENZENESULFONAMIDE DERIVATIVES

A novel benzenesulfonamide derivative represented by the formula has an inhibitory activity against phospholipase A2, so that it is effective in the treatment of diseases for which such an activity is efficacious

BENZENESULFONAMIDE DERIVATIVE

A novel benzenesulfonamide derivative of formula (I) which has an action of inhibiting phospholipase A2? and therefore is effective in treating diseases for which this action is used to advantage.